Survey of Anti-HIV and Anti-HCV Compounds from Natural Sources

Abstract

This review article describes our recent research on (from 2005 to the end of 2012) isolation and identification of natural products, their in vivo metabolites and synthesized derivatives as potential anti-viral agents. Bioactivity assays focused on the inhibition of essential viral enzymes such as HIV protease, HCV protease, and -glucosidase. Bioactive compounds were structurally classified as lignans, triterpenes, chlorogenic acid derivatives and farnesyl hydroquinones. The possible mechanisms of inhibition of a representative triterpene and a farnesyl hydroquinone on HIV-1 protease are discussed. We structurally modified some known triterpenes (betulinic, oleanolic, ursolic and glycyrrhetic acids, panaxadiol, panaxatriol) and chlorogenic acid to identify derivatives with improved inhibitory potency or improved selectivity for viral essential enzymes. Some novel structure-activity relationships (SARs) are also presented in this paper.

Anti-HIV and Anti-Candidal Effects of Methanolic Extract from Heteropterys brachiata

“…Other authors have focused on the structural modification of chlorogenic acid in order to potentiate its anti-HIV properties through the inhibition of the α-glucosidase. Besides the role of the inhibitors of α-glucosidase in the progression of diabetes by decreasing carbohydrate digestion and absorption, in recent years, the inhibition of α-glucosidase has been considered a promising strategy for the development of novel anti-HIV agents due to the glycosylation of viral envelope glycoproteins [30]. The envelope glycoproteins gp120 and gp41 play crucial roles in HIV entry, thus serving as key targets for the development of HIV entry inhibitors [31].…”

“…Inhibitors of α-glucosidases can cause glycoproteins to misfolded and remain within the endoplasmic reticulum, interfering with the viral life cycle and infectious process [32]. Thus, Hattori et al [30] proposed the utilization of novel α-glucosidase inhibitors through the optimization of the hydrophilicity of chlorogenic acid by addition of alkyl chains of various lengths. The addition of ketal or acetal bonds to chlorogenic acid derivatives caused an increase in the inhibitory activity of 1 α-glucosidases.…”